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Table 1 Pf TrxR inhibitory and antiplasmodial activities of tested compounds

From: Characterization of PfTrxR inhibitors using antimalarial assays and in silicotechniques

Test compounds PfTrxR IC50(μM)* Pf(D6) CQ sensitive IC50(μM)** SI D6 Pf(W2) CQ resistance IC50(μM)** SI W2 3T3 IC50(μM)
1,4-NQ 0.75 8.9 ± 2.3 4.6 16.7 ± 3.7 2.4 38.5 ± 0.76
2,4-DNPS 0.5 91.2 ± 11.3 0.8 72.3 ± 11.3 1.0 79 ± 3.51
4-NBT 2 8.3 ± 2.1 10 9.8 ± 1.9 8 80 ± 1.15
3-DAP 15.4 >100 >1 >100 >1 >100
MD 1.6 18.5 ± 1.9 3.8 28.3 ± 5.6 2.5 70.5 ± 3.69
CQ   0.055 ± 0.006   0.440 ± 0.045   NC
  1. *IC50 values, preparation of PfTrxR and optimal experimental conditions for the PfTrxR functional assay were reported in Andricopulo et al., 2006 [12]; Charvet et al., 2003 [13]; Munigunti et al., 2012 [14].
  2. **Values are mean ± S.D. of triplicate observations; SI: Selectivity index. NC: no cytotoxicity up to concentration much higher than the concentration responsible for its antiplasmodial activity.